Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos (e.g., Maytansinoids, Etc.) Patents (Class 514/229.5)
  • Patent number: 10259826
    Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lupus erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
    Type: Grant
    Filed: March 24, 2017
    Date of Patent: April 16, 2019
    Assignee: RIGEL PHARMACEUTICALS, INC.
    Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
  • Patent number: 10246467
    Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R7, A, V, W, X, Y, n, r and q are defined in claim 1, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases, and synthetic intermediates.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: April 2, 2019
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Juergen Ramharter, Joachim Broeker, Annika Gille, Andreas Gollner, Manuel Henry, Nina Kerres, Harald Weinstabl
  • Patent number: 10167298
    Abstract: The present invention relates to novel Pseudopolymorphs of Compound A, compositions comprising at least one Pseudopolymorph of Compound A, and methods of using the Pseudopolymorphs of Compound A for preparing compositions useful for treating or preventing HCV infection in a patient, wherein Compound A has the structure.
    Type: Grant
    Filed: October 24, 2014
    Date of Patent: January 1, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael McNevin, Yong Liu, Ian Mangion, Alfred Lee, Joyce Stellabott, Benjamin D. Sherry, Gary Martin, Kung-I Feng, Scott Schultz, Ryan Cohen, Yanfeng Zhang
  • Patent number: 10125148
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Grant
    Filed: February 19, 2014
    Date of Patent: November 13, 2018
    Assignee: ViiV HEALTHCARE UK (NO. 5) LIMITED
    Inventors: Timothy P. Connolly, Stanley D'Andrea, John F. Kadow, David R. Langley, B. Narasimhulu Naidu, Manoj Patel, Kevin Peese, Michael A. Walker, Zhongyu Wang, Zhizhen Barbara Zheng
  • Patent number: 9956227
    Abstract: The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.
    Type: Grant
    Filed: December 3, 2014
    Date of Patent: May 1, 2018
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Kimberly Vanover, Peng Li, Sharon Mates, Robert Davis, Lawrence P. Wennogle
  • Patent number: 9932353
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: April 3, 2018
    Assignee: ViiV HEALTHCARE UK (NO. 5) LIMITED
    Inventors: B. Narasimhulu Naidu, Manoj Patel
  • Patent number: 9872866
    Abstract: The present disclosure provides compositions that include a nanoparticle and a compound that increases the biological activity of the vitamin D receptor (VDR) (e.g., a VDR agonist), and methods of using such compounds to increase retention or storage of vitamin A, vitamin D, and/or lipids by a cell, such as an epithelial or stellate cell. Such methods can be used to treat or prevent fibrosis.
    Type: Grant
    Filed: October 23, 2015
    Date of Patent: January 23, 2018
    Assignees: Salk Institute for Biological Studies, The University of Sydney
    Inventors: Ning Ding, Michael Downes, Christopher Liddle, Ronald M. Evans
  • Patent number: 9839641
    Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.
    Type: Grant
    Filed: November 16, 2016
    Date of Patent: December 12, 2017
    Assignee: Entasis Therapeutics Limited
    Inventors: Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Hauck, Fei Zhou
  • Patent number: 9834566
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV integrase, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: December 5, 2017
    Assignee: ViiV HEALTHCARE UK (NO.5) LIMITED
    Inventors: John F. Kadow, B. Narasimhulu Naidu, Manoj Patel, Kevin Peese, Tao Wang, Zhiwei Yin, Zhongxing Zhang
  • Patent number: 9808471
    Abstract: Nasal pharmaceutical formulations comprising a drug substance having a specific particle size distribution profile are disclosed herein. Such profile provides increased bioavailability, increased efficacy or prolonged therapeutic effect of the drug substance when administered intranasally. The formulations of the present invention may comprise one or more corticosteroids having a specific particle size distribution profile. In a preferred embodiment, the corticosteroid is fluticasone or a pharmaceutically acceptable derivative thereof for the treatment of one or more symptoms of rhinitis. Preferably, the drug substance is fluticasone propionate. The formulations herein may be provided as an aqueous suspension suitable for inhalation via the intranasal route.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: November 7, 2017
    Assignee: Mylan Specialty LP
    Inventor: Imtiaz Chaudry
  • Patent number: 9540394
    Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.
    Type: Grant
    Filed: October 13, 2015
    Date of Patent: January 10, 2017
    Assignee: Entasis Therapeutics Limited
    Inventors: Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Hauck, Fei Zhou
  • Patent number: 9388166
    Abstract: The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) can be used as medicament.
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: July 12, 2016
    Assignee: Hoffman-La Roche Inc.
    Inventors: Zhi Chen, Shawn David Erickson
  • Patent number: 9321788
    Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.
    Type: Grant
    Filed: June 11, 2012
    Date of Patent: April 26, 2016
    Assignee: BASILEA PHARMACEUTICA AG
    Inventors: Berangere Gaucher, Franck Hubert Danel, Tong Xie, Lin Xu
  • Patent number: 9242998
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Grant
    Filed: February 3, 2014
    Date of Patent: January 26, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shuwen He, Xing Dai, Anandan Palani, Ravi Nargund, Zhong Lai, Nicolas Zorn, Dong Xiao, Qun Dang, Casey C. McComas, Peng Li, Xuanjia Peng, Richard Soll
  • Patent number: 9187495
    Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.
    Type: Grant
    Filed: October 16, 2014
    Date of Patent: November 17, 2015
    Assignee: Entasis Therapeutics Limited
    Inventors: Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
  • Publication number: 20150139915
    Abstract: Methods and compositions are described for reducing airway reactivity and the susceptibility to asthmatic bronchoconstriction that involve increasing sphingolipid content in airways and lungs of a mammalian subject.
    Type: Application
    Filed: May 16, 2013
    Publication date: May 21, 2015
    Inventors: Stefan Worgall, Tilla S. Worgall
  • Publication number: 20150057270
    Abstract: The invention provides prodrugs of DNA-reactive analogs of duocarmycin and CC-1065 anticancer agents, wherein a cyclic prodrug form, such as carbamate, thionocarbamate, or carbamimidate, can be hydrolyzed by the patient in vivo to yield a respective bioactive agent comprising a DNA-alkylating moiety and a binding/targeting moiety. The DNA-reactive moiety is a ?-spiro-cyclohexenone fused to a heterocyclyl group which can be produced by endogenous hydrolysis of a cyclic carbamate prodrug of the invention. The cyclic carbamate prodrug produces no residual byproduct during activation in vivo. Methods of synthesis and biological methods and data are also provided.
    Type: Application
    Filed: March 26, 2013
    Publication date: February 26, 2015
    Inventor: Dale L. Boger
  • Publication number: 20150025066
    Abstract: Compounds of the formula I in which A, L1, L2, X and Y have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis.
    Type: Application
    Filed: December 18, 2012
    Publication date: January 22, 2015
    Applicant: Merck Patent GmbH
    Inventors: Henry Yu, Lizbeth Celeste Deselm
  • Publication number: 20150018298
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, Y1, Y2, or L are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: July 11, 2014
    Publication date: January 15, 2015
    Inventors: Mingzhe Ji, Scott E. Lazerwith, Hyung-Jung Pyun
  • Patent number: 8927541
    Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: January 6, 2015
    Assignee: Basilea Pharmaceutica AG
    Inventors: Bérangère Gaucher, Franck Hubert Danel, XiaoHu Tang, Tong Xie, Lin Xu
  • Publication number: 20140364429
    Abstract: Provided are compounds antiviral compounds represented by formula Ia and Ib: that are highly potent as HCV NS5A inhibitors, where the structural variables are as defined herein. These compounds are useful in, for example, inhibiting Hepatitis C virus and treating Hepatitis C virus infections.
    Type: Application
    Filed: June 6, 2014
    Publication date: December 11, 2014
    Applicant: AB PHARMA LTD.
    Inventor: Zheng-Yun James ZHAN
  • Patent number: 8906929
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Grant
    Filed: August 5, 2013
    Date of Patent: December 9, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: B. Narasimhulu Naidu, Manoj Patel, Stanley D'Andrea, Zhizhen Barbara Zheng, Timothy P. Connolly, David R. Langley, Kevin Peese, Zhongyu Wang, Michael A. Walker, John F. Kadow
  • Patent number: 8889671
    Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: November 18, 2014
    Assignee: AstraZeneca AB
    Inventors: Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
  • Patent number: 8871759
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: October 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Steven W. Ludmerer, Kun Liu, Hao Wu, Richard Soll, Bin Zhong, Jian Zhu
  • Publication number: 20140303155
    Abstract: The invention relates to pharmacology and medicine, more particularly to novel pharmaceutical compositions and pharmaceutical kits for treating bacterial infections, and to novel method for treating diseases caused by bacterial infections including tuberculosis. The pharmaceutical composition is disclosed comprising Rifamycin and interferon inducer in pharmacologically effective doses, and also pharmaceutical kit for treating diseases caused by bacterial and healthcare acquired infections, comprising pharmacologically effective doses of Rifamycin in the form of a tablet, a capsule or an injection, interferon inducer in the form of a tablet, a capsule or an injection, and instruction for administration of the components of this pharmaceutical kit.
    Type: Application
    Filed: October 25, 2012
    Publication date: October 9, 2014
    Inventors: Alexandre Vasilievich Ivachtchenko, Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk
  • Publication number: 20140303144
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?2B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: October 9, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty
  • Publication number: 20140256717
    Abstract: There is provided compounds of formula I, wherein R1, R2a, R2b, R2c, X, Y, Z, R3 and ring A/B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K, PIM family kinase and/or mTOR) is desired and/or required, and particularly in the treatment of cancer. The invention also relates to combinations containing such compounds.
    Type: Application
    Filed: May 18, 2012
    Publication date: September 11, 2014
    Applicant: Centro Nacional de Investigaciones Oncológicas (CNIO)
    Inventors: Joaquín Pastor Fernández, Rosa Maria Álvarez Escobar, Rosario Concepción Riesco Fagundo, Ana Belén García García, Antonio Rodríguez Hergueta, Jose Ignacio Martin Hernando, Carmen Blanco Aparicio, David Álvaro Cebrián Muñoz
  • Publication number: 20140228353
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 14, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvvajit Chakravarty
  • Publication number: 20140221356
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: December 19, 2013
    Publication date: August 7, 2014
    Inventors: Haolun JIN, Scott E. LAZERWITH, Teresa Alejandra TREJO MARTIN, Elizabeth M. BACON, Jeromy J. COTTELL, Zhenhong R. CAI, Hyung-Jung PYUN, Philip Anthony MORGANELLI, Mingzhe JI, James G. TAYLOR, Xiaowu CHEN, Michael R. MISH, Manoj C. DESAI
  • Publication number: 20140221355
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, Z2, or Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: December 19, 2013
    Publication date: August 7, 2014
    Inventors: Scott E. LAZERWITH, Haolun JIN, Hyung-Jung Pyun
  • Publication number: 20140213571
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 20, 2012
    Publication date: July 31, 2014
    Inventors: Nigel J. Liverton, Casey Cameron McComas, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Shuwen He, Xing Dai, Hong Liu, Zhong Lai, Clare London, Dong Xiao, Nicolas Zorn, Ravi Nargund
  • Publication number: 20140206677
    Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.
    Type: Application
    Filed: January 21, 2014
    Publication date: July 24, 2014
    Applicant: AstraZeneca AB
    Inventors: Gregory Steven BASARAB, Madhusudhan Reddy GOWRAVARAM, Sheila Irene HAUCK, Fei ZHOU
  • Publication number: 20140206663
    Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: March 19, 2014
    Publication date: July 24, 2014
    Inventors: Jianfei Wang, Eric C. Breinlinger, Martine Barth, Michael M. Friedman, Fabrice Guillier, Maria A. Argiriadi, Jeremy Edmunds, Dominique Potin, Adrian D. Hobson, Wentao Wu, Dominique Bonafoux, Didier Thomas, Dawn M. George, Linlin Dai, Yang Zhang
  • Publication number: 20140199264
    Abstract: The present invention relates to novel Tetracyclic Xanthene Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, Y1, Y2, Z, Ra, Rb, R1a, R1b and R2 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Xanthene Derivative, and methods of using the Tetracyclic Xanthene Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: March 16, 2012
    Publication date: July 17, 2014
    Inventors: Craig A. Coburn, Stuart B. Rosenblum, Joseph A. Kozlowski, Richard Soll, Hao Wu, Bin Hu, Bin Zhong, Dahai Wang, Changmao Shen, Fei Sun
  • Publication number: 20140200209
    Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
    Type: Application
    Filed: March 14, 2014
    Publication date: July 17, 2014
    Applicants: ViiV Healthcare Company, Shionogi & Co., Ltd.
    Inventors: Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
  • Publication number: 20140163021
    Abstract: Candidate compounds for use in neuro-protection and repair in neurological disorders involving Tau dysfunction (including Alzheimer's disease) are identified from a direct interaction between proteins FKBP52 and Tau. The method for screening a drug for the prevention and treatment of neurological disorders involving Tau dysfunction includes determining the ability of a candidate compound, to modulate binding between a Tau polypeptide and a FKBP52 polypeptide, and selecting positively the candidate compound that modulates binding.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 12, 2014
    Applicant: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Etienne Baulieu, Beatrice Chambraud
  • Patent number: 8748464
    Abstract: The present disclosure provides a method of increasing an immune response in an individual, the method involving administering to an individual in need thereof an inhibitor of SIRT1. The present disclosure provides a method of reducing an immune response, e.g., to treat chronic immune hyperactivity, the method generally involving administering to an individual in need thereof an activator of SIRT1. The present disclosure provides a method of modulating activation and differentiation of CD4+ T cells.
    Type: Grant
    Filed: July 16, 2010
    Date of Patent: June 10, 2014
    Assignee: The J. David Gladstone Institutes
    Inventors: Eric M. Verdin, Melanie Ott, Hye-Sook Kwon, Hyungwook Lim
  • Publication number: 20140128371
    Abstract: The present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.
    Type: Application
    Filed: January 13, 2014
    Publication date: May 8, 2014
    Applicant: ASTRAZENECA AB
    Inventors: Kevin BARVIAN, Gregory Steven BASARAB, Madhusudhan Reddy GOWRAVARAM, Sheila Irene HAUCK, Fei ZHOU
  • Patent number: 8685965
    Abstract: Compounds of Formula (I), (wherein variables A1, A2, A3, A4, A5, A6, A7, A8, L, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG, W, Y and Z are as described herein) useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP receptors are involved.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: April 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Donnette D. Staas, Ian M. Bell, Harold G. Selnick
  • Publication number: 20140080821
    Abstract: Provided herein are benzopyrimido-pyrrolo-oxazine-dione (BPO) compounds and pyrimido-pyrrolo-quinoxalinedione (PPQ) compounds, and compositions comprising these compounds, that inhibit cystic fibrosis transmembrane conductance regulator (CFTR) mediated ion transport and that are useful for treating diseases and disorders associated with aberrantly increased CFTR chloride channel activity, such as polycystic kidney disease and secretory diarrheas. The compounds and compositions comprising the compounds described herein may be used for inhibiting expansion or preventing formation of cysts in persons who have polycystic kidney disease.
    Type: Application
    Filed: May 25, 2012
    Publication date: March 20, 2014
    Applicant: The Regents of the University of California
    Inventors: Alan S. Verkman, David S. Snyder
  • Publication number: 20140072536
    Abstract: Disclosed herein are ?7?1 integrin modulatory agents and methods of using such to treat conditions associated with decreased ?7?1 integrin expression or activity, including muscular dystrophy. In one example, methods for treating a subject with muscular dystrophy are disclosed. The methods include administering an effective amount of an ?7?1 integrin modulatory agent to the subject with muscular dystrophy, wherein the ?7?1 integrin modulatory agent increases ?7?1 integrin expression or activity as compared to ?7?1 integrin expression or activity prior to treatment, thereby treating the subject with muscular dystrophy. Also disclosed are methods of enhancing muscle regeneration, repair, or maintenance in a subject and methods of enhancing ?7?1 integrin expression by use of the disclosed ?7?1 integrin modulatory agents. Methods of prospectively preventing or reducing muscle injury or damage in a subject are also disclosed.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 13, 2014
    Applicant: Board of Regents of the Nevada System of Higher Education On Behalf of the University of Nevada
    Inventors: Ryan Wuebbles, Dean Burkin
  • Publication number: 20140051692
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Application
    Filed: August 5, 2013
    Publication date: February 20, 2014
    Inventors: B. Narasimhulu Naidu, Manoj Patel, Stanley D'Andrea, Zhizhen Barbara Zheng, Timothy P. Connolly, David R. Langley, Kevin Peese, Zhongyu Wang, Michael A. Walker, John F. Kadow
  • Publication number: 20140050783
    Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals and pharmaceutical compositions comprising them for the treatment of one or more disorders involving the 5-HT2A, SERT and/or dopamine D2 pathways are disclosed. In addition, the compounds may be combined with other therapeutic agents for the treatment of one or more sleep disorders, depression, psychosis, dyskinesias, and/or Parkinson's disease or any combinations.
    Type: Application
    Filed: October 30, 2013
    Publication date: February 20, 2014
    Applicant: INTRA-CELLULAR THERAPIES INC.
    Inventors: Sharon MATES, Allen FIENBERG, Lawrence P. WENNOGLE
  • Patent number: 8624003
    Abstract: This invention describes a method of conjugating a cell binding agent such as an antibody with an effector group (e.g., a cytotoxic agent) or a reporter group (e.g., a radionuclide), whereby the reporter or effector group is first reacted with a bifunctional linker and the mixture is then used without purification for the conjugation reaction with the cell binding agent. The method described in this invention is advantageous for preparation of stably-linked conjugates of cell binding agents, such as antibodies with effector or reporter groups. This conjugation method provides in high yields conjugates of high purity and homogeneity that are without inter-chain cross-linking and inactivated linker residues.
    Type: Grant
    Filed: June 3, 2010
    Date of Patent: January 7, 2014
    Assignee: ImmunoGen, Inc.
    Inventors: Brenda A. Kellogg, Rajeeva Singh, Ravi V. J. Chari
  • Patent number: 8598119
    Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals and pharmaceutical compositions comprising them for the treatment of one or more disorders involving the 5-HT2A, SERT and/or dopamine D2 pathways are disclosed. In addition, the compounds may be combined with other therapeutic agents for the treatment of one or more sleep disorders, depression, psychosis, dyskinesias, and/or Parkinson's disease or any combinations.
    Type: Grant
    Filed: May 27, 2009
    Date of Patent: December 3, 2013
    Assignee: Intra-Cellular Therapies, Inc.
    Inventors: Sharon Mates, Allen Fienberg, Lawrence Wennogle
  • Patent number: 8598164
    Abstract: The invention relates to heterocyclic chromene-spirocyclic piperidine amides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: December 3, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Sabina Hadida-Ruah, Edward Adam Kallel, Mark Thomas Miller, Joseph Pontillo, Vijayalaksmi Arumugam, Nicole Hilgraf, Jason McCartney, Peter Diederik Jan Grootenhuis, Corey Anderson, Mehdi Numa, Bryan A. Frieman, Brian Richard Bear, James Philip Johnson, Jr.
  • Publication number: 20130302416
    Abstract: New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase.
    Type: Application
    Filed: January 19, 2012
    Publication date: November 14, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldarelli, Francesco Casuscelli, Daniele Donati, Danilo Mirizzi, Francesca Quartieri, Marco Silvagni
  • Patent number: 8557806
    Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
    Type: Grant
    Filed: March 13, 2012
    Date of Patent: October 15, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li
  • Patent number: 8546384
    Abstract: Naphthalimide compounds are used in tissue bonding and protein cross-linking applications. When activated by an activating agent, such as light in the 400-500 nm absorption range, the naphthalimide compounds form chemically-reactive species that cross-link proteins, bond connective tissues together, and bond tissues and other biomaterials together. A naphthalimide-labeled biomolecule, such as a naphthalimide-labeled chitosan, is also capable of bonding tissues without subsequent direct illumination of the contacted tissue area. The naphthalimide compounds may be used in tissue or arterial repair, stabilization of an expanded arterial wall after angioplasty, tethering pharmaceutical agents to tissue surfaces to provide local drug delivery, and for chemically bonding skin care products, sunscreens, and cosmetics to the skin.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: October 1, 2013
    Assignee: Alumend, LLC
    Inventors: Ronald E. Utecht, Kaia L. Kloster, Millard M. Judy, Kevin J. Vaska, James L. Matthews
  • Patent number: 8546383
    Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)— group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
    Type: Grant
    Filed: May 25, 2012
    Date of Patent: October 1, 2013
    Assignee: 3M Innovative Properties Company
    Inventors: George W. Griesgraber, Tushar A. Kshirsagar, Azim A. Celebi, Sarah J. Slania, Michael E. Danielson, Michael J. Rice, Joshua R. Wurst